Tag: M.W=150-200

Smith, Samuel M. published the artcileScope, Limitations and Mechanistic Analysis of the HyperBTM-Catalyzed Acylative Kinetic Resolution of Tertiary Heterocyclic Alcohols, Safety of 4-Methoxyphenylacetic acid, the main research area is tertiary heterocyclic alc preparation enantioselective; hydroxyoxindole hydroxylactam acylative kinetic resolution HyperBTM isothiourea catalyst.

The full scope and limitations of the catalytic acylative kinetic resolution of a range of tertiary heterocyclic alcs. (78 examples, s up to >200) is reported under operationally-simple conditions, using low loadings of a com. available Lewis basic isothiourea catalyst, HyperBTM (generally 1 mol %). The protocol is highly effective for the kinetic resolution of 3-substituted 3-hydroxyoxindole and α-substituted α-hydroxylactam derivatives bearing up to three potential recognition motifs at the stereogenic tertiary carbinol center. The full power of this methodol. has been showcased through the synthesis of highly enantioenriched biol.-active target compounds in both enantiomeric forms. To provide further insight into the reaction mechanism, a detailed kinetic anal. of this Lewis base-catalyzed acylation of tertiary alcs. is reported using the variable time normalization anal. (VTNA) method.

European Journal of Organic Chemistry published new progress about Acylation catalysts (stereoselective). 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Safety of 4-Methoxyphenylacetic acid.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Bi, Tongyu published the artcileNatural scaffolds-inspired synthesis of CF3-substituted macrolides enabled by Rh-catalyzed C-H alkylation macrocyclization, Recommanded Product: 4-Methoxyphenylacetic acid, the main research area is trifluoromethyl macrolide preparation diastereoselective chemoselective antiinflammatory.

Inspired by the key scaffolds of rapamycin and FR252921, a Rh(III)-catalyzed C-H alkylation macrocyclization, which enables access to CF3-substituted macrolides, is reported. DFT calculations revealed that the chemoselectivity between C-H alkylation and olefination macrocyclization is highly controllable. Moreover, the unique CF3-substituted macrolides showed potent anti-inflammation activities against TNF-α, IL-6 and CCL2 mRNA expression.

Chinese Chemical Letters published new progress about Alkylation catalysts (chemoselective). 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Recommanded Product: 4-Methoxyphenylacetic acid.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Lin, Hua-Chen published the artcileA Pd-H/Isothiourea Cooperative Catalysis Approach to anti-Aldol Motifs: Enantioselective α-Alkylation of Esters with Oxyallenes, Formula: C9H10O3, the main research area is oxyallene pentafluorophenyl acetate palladium benzotetramisole enantioselective diastereoselective alkylation; pentafluorophenyl oxypentenoate preparation; methyl oxy butenyl carbamate preparation; Allenes; C1-Ammonium Enolates; Enantioselectivity; Isothioureas; Palladium Catalysis.

To complement the array of substrate-based strategies, and regulate enolate geometry at the catalyst level, a direct catalytic alkylation of esters with oxyallenes was developed. Synergizing metal hydride reactivity with Lewis base catalysis resulted in a broad reaction scope with useful levels of stereocontrol (up to >99% ee). Facile derivatization of these ambiphilic linchpins was demonstrated, providing access to high-value vicinal stereocenter-containing motifs, including 1,2-amino alcs.

Angewandte Chemie, International Edition published new progress about Alkylation catalysts, stereoselective. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Formula: C9H10O3.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Arokianathar, Jude N. published the artcileIsothiourea-Catalyzed Enantioselective α-Alkylation of Esters via 1,6-Conjugate Addition to para-Quinone Methides, Recommanded Product: 4-Methoxyphenylacetic acid, the main research area is alkylated ester enantioselective diastereoselective preparation; nitrophenyl ester isothiourea catalyzed enantioselective alkylation para quinone methide; 1,6-conjugate addition; ammonium enolate; aryloxide; ester functionalization; isothiourea; quinone methide.

The isothiourea-catalyzed enantioselective 1,6-conjugate addition of para-nitrophenyl esters to 2,6-disubstituted para-quinone methides was reported. Para-nitrophenoxide, generated in situ from initial N-acylation of the isothiourea by the para-nitrophenyl ester, was proposed to facilitate catalyst turnover in this transformation. A range of para-nitrophenyl ester products could be isolated, or derivatized in situ by addition of benzylamine to give amides at up to 99% yield. Although low diastereocontrol was observed, the diastereoisomeric ester products were separable and formed with high enantiocontrol (up to 94:6 er).

Molecules published new progress about Alkylation catalysts, stereoselective. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Recommanded Product: 4-Methoxyphenylacetic acid.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Chen, Hongyu published the artcileData-driven catalyst optimization for stereodivergent asymmetric synthesis by iridium/boron hybrid catalysis, Application In Synthesis of 104-01-8, the main research area is allylic carboxylic acid stereodivergent enantioselective regioselective chemoselective diastereoselective preparation; carboxylic acid stereodivergent enantioselective allylation iridium boron hybrid catalysis.

Here, the straightforward identification of asym. two-component iridium/boron hybrid catalyst systems for α-C-allylation of carboxylic acids was reported. Structural optimization of the chiral ligands for iridium catalysts was driven by mol.-field-based regression anal. with a dataset containing overall 32 mol. structures. The catalyst systems enabled selective access to all the possible isomers of chiral carboxylic acids bearing contiguous stereocenters. This chemoselective and stereodivergent, asym. catalysis was applicable to late-stage structural modifications of drugs and their derivatives

Cell Reports Physical Science published new progress about Allylation catalysts, stereoselective. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Application In Synthesis of 104-01-8.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Ali, Mahboob published the artcileChalcones: As Potent α-amylase Enzyme Inhibitors; Synthesis, In Vitro, and In Silico Studies, Application In Synthesis of 86-51-1, the main research area is chalcone alpha amylase enzyme inhibitory potential; Chalcones; diabetes mellitus; in vitro; molecular docking.; synthesis; α-amylase enzyme inhibition.

The inhibition of α-amylase enzyme is one of the best therapeutic approach for the management of type II diabetes mellitus. Chalcone possesses a wide range of biol. activities. In the current study chalcone derivatives (1-16) were synthesized and evaluated their inhibitory potential against α-amylase enzyme. For that purpose, a library of substituted (E)-1-(naphthalene-2-yl)-3-phenylprop-2-en-1-ones was synthesized by Claisen-Schmidt condensation reaction of 2-acetonaphthanone and substituted aryl benzaldehyde in the presence of base and characterized via different spectroscopic techniques such as EI-MS, HRESI-MS, 1H-, and 13C-NMR. Sixteen synthetic chalcones were evaluated for in vitro porcine pancreatic α-amylase inhibition. All the chalcones demonstrated good inhibitory activities in the range of IC50 = 1.25 ± 1.05 to 2.40 ± 0.09 μM as compared to the standard com. drug acarbose (IC50 = 1.34 ± 0.3 μM). Chalcone derivatives (1-16) were synthesized, characterized, and evaluated for their α-amylase inhibition. SAR revealed that electron donating groups in the Ph ring have more influence on enzyme inhibition. However, to insight the participation of different substituents in the chalcones on the binding interactions with the α-amylase enzyme, in silico (computer simulation) mol. modeling analyses were carried out.

Medicinal Chemistry (Sharjah, United Arab Emirates) published new progress about Claisen-Schmidt condensation reaction. 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, Application In Synthesis of 86-51-1.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Mak, Jeffrey Y. W. published the artcileHDAC7 Inhibition by Phenacetyl and Phenylbenzoyl Hydroxamates, Application of 4-Methoxyphenylacetic acid, the main research area is HDAC7 inhibitors catalytic site phenylbenzoyl hydroxamates phthalimide stability solubility.

The zinc-containing histone deacetylase enzyme HDAC7 is emerging as an important regulator of immunometabolism and cancer. Here, we exploit a cavity in HDAC7, filled by Tyr303 in HDAC1, to derive new inhibitors. Phenacetyl hydroxamates and 2-phenylbenzoyl hydroxamates bind to Zn2+ and are 50-2700-fold more selective inhibitors of HDAC7 than HDAC1. Phenylbenzoyl hydroxamates are 30-70-fold more potent HDAC7 inhibitors than phenacetyl hydroxamates, which is attributed to the benzoyl aromatic group interacting with Phe679 and Phe738. Phthalimide capping groups, including a saccharin analog, decrease rotational freedom and provide hydrogen bond acceptor carbonyl/sulfonamide oxygens that increase inhibitor potency, liver microsome stability, solubility, and cell activity. Despite being the most potent HDAC7 inhibitors to date, they are not selective among class IIa enzymes. These strategies may help to produce tools for interrogating HDAC7 biol. related to its catalytic site.

Journal of Medicinal Chemistry published new progress about Drug metabolism (metabolic stability). 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Application of 4-Methoxyphenylacetic acid.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Lee, Jisook published the artcileNovel Human Aminopeptidase N Inhibitors: Discovery and Optimization of Subsite Binding Interactions, Recommanded Product: 4-Methoxyphenylacetic acid, the main research area is microsomal aminopeptidase N hydroxamic acid.

Aminopeptidase N (APN/CD13) is a zinc-dependent M1 aminopeptidase that contributes to cancer progression by promoting angiogenesis, metastasis, and tumor invasion. We have previously identified hydroxamic acid-containing analogs that are potent inhibitors of the APN homolog from the malarial parasite Plasmodium falciparum M1 aminopeptidase (PfA-M1). Herein, we describe the rationale that underpins the repurposing of PfA-M1 inhibitors as novel APN inhibitors. A series of novel hydroxamic acid analogs were developed using a structure-based design approach and evaluated their inhibition activities against APN. N-(2-(Hydroxyamino)-2-oxo-1-(3′,4′,5′-trifluoro-[1,1′-biphenyl]-4-yl)ethyl)-4-(methylsulfonamido)benzamide (6ad) proved to be an extremely potent inhibitor of APN activity in vitro, selective against other zinc-dependent enzymes such as matrix metalloproteases, and possessed limited cytotoxicity against Ad293 cells and favorable physicochem. and metabolic stability properties. The combined results indicate that compound 6ad may be a useful lead for the development of anticancer agents.

Journal of Medicinal Chemistry published new progress about Drug metabolism (metabolic stability). 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Recommanded Product: 4-Methoxyphenylacetic acid.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Chen, Si-Qi published the artcileAldehyde as a Traceless Directing Group for Regioselective C-H Alkylation Catalyzed by Rhodium(III) in Air, Product Details of C9H10O3, the main research area is aromatic aldehyde acrylate regioselective decarbonylative alkylation rhodium catalyst air.

The aromatic aldehyde as a traceless directing group for the regioselective C-H alkylation catalyzed by rhodium(III) under aerobic atm. conditions has been developed. The process involves an aldehyde assisted direct addition of C-H bond to unsaturated electrophiles of acrylates or acrylic acids, and the subsequent decarbonylation. A trace amount of water is found to favor the reaction.

Organic Letters published new progress about Alkylation catalysts, regioselective. 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, Product Details of C9H10O3.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Zhao, Yunbo published the artcileB(C6F5)3-Catalyzed site-selective N1-alkylation of benzotriazoles with diazoalkanes, Recommanded Product: 4-Methoxyphenylacetic acid, the main research area is diazoacetate benzotriazole pentafluorophenyl borane catalyst regioselective alkylation; alkyl benzotriazole preparation.

Alkylation of benzotriazoles is synthetically challenging, often leading to mixtures of N1 and N2 alkylation. Herein, metal-free catalytic site-selective N1-alkylation of benzotriazoles with diazoalkanes was described in the presence of 10 mol% of B(C6F5)3. These reactions provide N1-alkylated benzotriazoles in good to excellent yields and this protocol was successfully adapted to gram-scale syntheses as well as a derivative with antimicrobial activity.

Chemical Communications (Cambridge, United Kingdom) published new progress about Alkylation catalysts, regioselective. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Recommanded Product: 4-Methoxyphenylacetic acid.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem